Literature DB >> 24461295

A novel class of ion displacement ligands as antagonists of the αIIbβ3 receptor that limit conformational reorganization of the receptor.

Jian-kang Jiang1, Joshua G McCoy1, Min Shen1, Christopher A LeClair1, Wenwei Huang1, Ana Negri2, Jihong Li3, Robert Blue3, Amanda Weil Harrington3, Sarasija Naini3, George David3, Won-Seok Choi3, Elisabetta Volpi3, Joseph Fernandez4, Mariana Babayeva5, Mark A Nedelman6, Marta Filizola2, Barry S Coller3, Craig J Thomas7.   

Abstract

A collection of αIIbβ3 integrin receptor antagonists possessing a unique MIDAS metal ion displacement mechanism of action is presented. Insight into these agents' structure-activity relationships, binding modality, and pharmacokinetic and pharmacodynamic profiles highlight the potential of these small molecule ion displacement ligands as attractive candidates for clinical development. Published by Elsevier Ltd.

Entities:  

Keywords:  Ion displacement ligand; Platelet; αIIbβ3 Integrin receptor

Mesh：

Substances：

Year:  2014        PMID： 24461295      PMCID： PMC3951875          DOI： 10.1016/j.bmcl.2013.12.122

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN： 0960-894X            Impact factor:   2.940


  23 in total

1.  Global conformational rearrangements in integrin extracellular domains in outside-in and inside-out signaling.

Authors:  Junichi Takagi; Benjamin M Petre; Thomas Walz; Timothy A Springer
Journal:  Cell       Date:  2002-09-06       Impact factor: 41.582

2.  Treatment with tirofiban for acute coronary syndrome (ACS): a systematic review and network analysis.

Authors:  S H Lang; N Manning; N Armstrong; K Misso; A Allen; M Di Nisio; J Kleijnen
Journal:  Curr Med Res Opin       Date:  2012-01-31       Impact factor: 2.580

3.  Closed headpiece of integrin αIIbβ3 and its complex with an αIIbβ3-specific antagonist that does not induce opening.

Authors:  Jieqing Zhu; Jianghai Zhu; Ana Negri; Davide Provasi; Marta Filizola; Barry S Coller; Timothy A Springer
Journal:  Blood       Date:  2010-08-02       Impact factor: 22.113

Review 4.  Structural basis of integrin regulation and signaling.

Authors:  Bing-Hao Luo; Christopher V Carman; Timothy A Springer
Journal:  Annu Rev Immunol       Date:  2007       Impact factor: 28.527

5.  In-ambulance abciximab administration in STEMI patients prior to primary PCI is associated with smaller infarct size, improved LV function and lower incidence of heart failure: results from the Leiden MISSION! acute myocardial infarction treatment optimization program.

Authors:  Ayman K M Hassan; Su San Liem; Frank van der Kley; Sandrin C Bergheanu; Ron Wolterbeek; Jan Bosch; Marianne Bootsma; Katja Zeppenfeld; Arnoud van der Laarse; Douwe E Atsma; J Wouter Jukema; Martin J Schalij
Journal:  Catheter Cardiovasc Interv       Date:  2009-08-01       Impact factor: 2.692

6.  Structure-guided design of a high-affinity platelet integrin αIIbβ3 receptor antagonist that disrupts Mg²⁺ binding to the MIDAS.

Authors:  Jieqing Zhu; Won-Seok Choi; Joshua G McCoy; Ana Negri; Jianghai Zhu; Sarasija Naini; Jihong Li; Min Shen; Wenwei Huang; Daniel Bougie; Mark Rasmussen; Richard Aster; Craig J Thomas; Marta Filizola; Timothy A Springer; Barry S Coller
Journal:  Sci Transl Med       Date:  2012-03-14       Impact factor: 17.956

7.  Early glycoprotein IIb-IIIa inhibitors in primary angioplasty-abciximab long-term results (EGYPT-ALT) cooperation: individual patient's data meta-analysis.

Authors:  G DE Luca; F Bellandi; K Huber; M Noc; A S Petronio; H-R Arntz; M Maioli; H M Gabriel; S Zorman; M DE Carlo; T Rakowski; M Gyongyosi; D Dudek
Journal:  J Thromb Haemost       Date:  2011-12       Impact factor: 5.824

8.  Efficacy and safety of early versus late glycoprotein IIb/IIIa inhibitors for PCI.

Authors:  Qiang Xu; Jian Yin; Liang-yi Si
Journal:  Int J Cardiol       Date:  2012-07-04       Impact factor: 4.164

9.  Integrin priming dynamics: mechanisms of integrin antagonist-promoted alphaIIbbeta3:PAC-1 molecular recognition.

Authors:  Roy R Hantgan; Mary C Stahle
Journal:  Biochemistry       Date:  2009-09-08       Impact factor: 3.162

10.  Structural and therapeutic insights from the species specificity and in vivo antithrombotic activity of a novel alphaIIb-specific alphaIIbbeta3 antagonist.

Authors:  Robert Blue; M Anna Kowalska; Jessica Hirsch; Marta Murcia; Christin A Janczak; Amanda Harrington; Marketa Jirouskova; Jihong Li; Rudy Fuentes; Michael A Thornton; Marta Filizola; Mortimer Poncz; Barry S Coller
Journal:  Blood       Date:  2009-05-04       Impact factor: 22.113
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  4 in total

1.  RUC-4: a novel αIIbβ3 antagonist for prehospital therapy of myocardial infarction.

Authors:  Jihong Li; Spandana Vootukuri; Yi Shang; Ana Negri; Jian-Kang Jiang; Mark Nedelman; Thomas G Diacovo; Marta Filizola; Craig J Thomas; Barry S Coller
Journal:  Arterioscler Thromb Vasc Biol       Date:  2014-08-21       Impact factor: 8.311

2.  The platelet: life on the razor's edge between hemorrhage and thrombosis.

Authors:  Barry S Coller
Journal:  Transfusion       Date:  2014-08-05       Impact factor: 3.157

3.  Morphometric analysis of spread platelets identifies integrin αIIbβ3-specific contractile phenotype.

Authors:  Sebastian Lickert; Simona Sorrentino; Jan-Dirk Studt; Ohad Medalia; Viola Vogel; Ingmar Schoen
Journal:  Sci Rep       Date:  2018-04-03       Impact factor: 4.379

4.  Preclinical Studies of RUC-4, a Novel Platelet αIIbβ3 Antagonist, in Non-Human Primates and With Human Platelets.

Authors:  Spandana Vootukuri; Jihong Li; Mark Nedelman; Craig Thomas; Jiang-Kang Jiang; Mariana Babayeva; Barry S Coller
Journal:  J Clin Transl Sci       Date:  2019-06-28
  4 in total

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